MELARSOPROL

ID: ALA166

Max Phase: Phase

Molecular Formula: C12H15AsN6OS2

Molecular Weight: 398.35

Molecule Type: Small molecule

Associated Items:

Representations

Synonyms (4): Mel b | Melarsoprol | RP 3854 | RP-3854
Synonyms from Alternative Forms(4):

    Canonical SMILES:  Nc1nc(N)nc(Nc2ccc([As]3SCC(CO)S3)cc2)n1

    Standard InChI:  InChI=1S/C12H15AsN6OS2/c14-10-17-11(15)19-12(18-10)16-8-3-1-7(2-4-8)13-21-6-9(5-20)22-13/h1-4,9,20H,5-6H2,(H5,14,15,16,17,18,19)

    Standard InChI Key:  JCYZMTMYPZHVBF-UHFFFAOYSA-N

    Associated Targets(Human)

    MRC5 9203 Activities

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    HL-60 67320 Activities

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    HT-29 80576 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Cathepsin B 3822 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Liver microsome 8277 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Plasma 7708 Activities

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    Homo sapiens 32628 Activities

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    Dopamine D1 receptor 9720 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    HERG 29587 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Dopamine transporter 10535 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Estrogen receptor alpha 17718 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Acetylcholinesterase 18204 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Norepinephrine transporter 10102 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Serotonin transporter 12625 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Alpha-2a adrenergic receptor 9450 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Mu opioid receptor 19785 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Monoamine oxidase A 11911 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Serotonin 1a (5-HT1a) receptor 14969 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Phosphodiesterase 3A 3309 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Dopamine D3 receptor 14368 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Muscarinic acetylcholine receptor M2 10671 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Thrombin 11687 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Thromboxane A2 receptor 5717 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Adenosine A3 receptor 15931 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Histamine H3 receptor 10389 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Serotonin 2b (5-HT2b) receptor 10323 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Adenosine A1 receptor 17603 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Androgen Receptor 11781 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Progesterone receptor 8562 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Cyclooxygenase-1 9233 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Phosphodiesterase 4A 1943 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Alpha-1a adrenergic receptor 8359 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Muscarinic acetylcholine receptor M1 12690 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Associated Targets(non-human)

    Mus musculus 284745 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Trypanosoma brucei rhodesiense 7991 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    L6 7924 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Trypanosoma brucei 78846 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Trypanosoma cruzi 99888 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Nucleoside transporter 2 17 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Trypanosoma brucei brucei 13300 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Leishmania donovani 89745 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Trichomonas vaginalis 2376 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    J774 3120 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Rhodesain 1463 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Plasmodium falciparum 966862 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Giardia intestinalis 1290 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Babesia divergens 18 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Trypanosoma brucei gambiense 523 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Liver 8163 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Plasma 6361 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Rattus norvegicus 775804 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    GABA receptor alpha-1 subunit 2848 Activities

    Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

    Molecule Features

    Natural Product: NoOral: NoChemical Probe: NoParenteral: No
    Molecule Type: Small moleculeTopical: NoFirst In Class: NoBlack Box: No
    Chirality: NoAvailability: NoProdrug: Yes

    Drug Indications

    MESH IDMESH Heading EFO IDsEFO TermsMax Phase for IndicationReferences

    Mechanisms of Action

    Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

    Properties

    Molecular Weight: 398.35Molecular Weight (Monoisotopic): 397.9965AlogP: #Rotatable Bonds:
    Polar Surface Area: Molecular Species: HBA: HBD:
    #RO5 Violations: HBA (Lipinski): HBD (Lipinski): #RO5 Violations (Lipinski):
    CX Acidic pKa: CX Basic pKa: CX LogP: CX LogD:
    Aromatic Rings: Heavy Atoms: QED Weighted: Np Likeness Score:

    References

    1. Dardonville C, Brun R..  (2004)  Bisguanidine, bis(2-aminoimidazoline), and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation.,  47  (9): [PMID:15084128] [10.1021/jm031024u]
    2. Girault S, Grellier P, Berecibar A, Maes L, Mouray E, Lemière P, Debreu MA, Davioud-Charvet E, Sergheraert C..  (2000)  Antimalarial, antitrypanosomal, and antileishmanial activities and cytotoxicity of bis(9-amino-6-chloro-2-methoxyacridines): influence of the linker.,  43  (14): [PMID:10893302] [10.1021/jm990946n]
    3. Wright AD, Goclik E, König GM, Kaminsky R..  (2002)  Lepadins D-F: antiplasmodial and antitrypanosomal decahydroquinoline derivatives from the tropical marine tunicate Didemnum sp.,  45  (14): [PMID:12086492] [10.1021/jm0110892]
    4. Millet R, Maes L, Landry V, Sergheraert C, Davioud-Charvet E..  (2002)  Antitrypanosomal activities and cytotoxicity of 5-nitro-2-furancarbohydrazides.,  12  (24): [PMID:12443785] [10.1016/s0960-894x(02)00788-6]
    5. Chowdhury SF, Villamor VB, Guerrero RH, Leal I, Brun R, Croft SL, Goodman JM, Maes L, Ruiz-Perez LM, Pacanowska DG, Gilbert IH..  (1999)  Design, synthesis, and evaluation of inhibitors of trypanosomal and leishmanial dihydrofolate reductase.,  42  (21): [PMID:10543874] [10.1021/jm981130+]
    6. Ulrich P, Cerami A..  (1982)  Potential antitrypanosomal agents. 1,N2-Disubstituted 2-amino-5-hydroxy-4-methylnaphtho[1,2-d]thiazolium salts and related compounds.,  25  (6): [PMID:7097719] [10.1021/jm00348a009]
    7. Baliani A, Bueno GJ, Stewart ML, Yardley V, Brun R, Barrett MP, Gilbert IH..  (2005)  Design and synthesis of a series of melamine-based nitroheterocycles with activity against Trypanosomatid parasites.,  48  (17): [PMID:16107157] [10.1021/jm050177+]
    8. Hui X, Desrivot J, Bories C, Loiseau PM, Franck X, Hocquemiller R, Figadère B..  (2006)  Synthesis and antiprotozoal activity of some new synthetic substituted quinoxalines.,  16  (4): [PMID:16309903] [10.1016/j.bmcl.2005.11.025]
    9. Vicik R, Hoerr V, Glaser M, Schultheis M, Hansell E, McKerrow JH, Holzgrabe U, Caffrey CR, Ponte-Sucre A, Moll H, Stich A, Schirmeister T..  (2006)  Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.,  16  (10): [PMID:16516467] [10.1016/j.bmcl.2006.02.026]
    10. Berger H, Seebacher W, Saf R, Kaiser M, Brun R, Weis R..  (2006)  Antiprotozoal activities of new bis-chlorophenyl derivatives of bicyclic octanes and aza-nonanes.,  16  (20): [PMID:16889962] [10.1016/j.bmcl.2006.07.057]
    11. Hay AE, Ioset JR, Ahua KM, Diallo D, Brun R, Hostettmann K..  (2007)  Limonoid orthoacetates and antiprotozoal compounds from the roots of Pseudocedrela kotschyi.,  70  (1): [PMID:17253841] [10.1021/np0680230]
    12. Patrick DA, Bakunov SA, Bakunova SM, Kumar EV, Lombardy RJ, Jones SK, Bridges AS, Zhirnov O, Hall JE, Wenzler T, Brun R, Tidwell RR..  (2007)  Synthesis and in vitro antiprotozoal activities of dicationic 3,5-diphenylisoxazoles.,  50  (10): [PMID:17439202] [10.1021/jm0612867]
    13. Schlapper C, Seebacher W, Kaiser M, Brun R, Saf R, Weis R..  (2007)  Bicyclo[2.2.2]octyl esters of dialkylamino acids as antiprotozoals.,  15  (16): [PMID:17544672] [10.1016/j.bmc.2007.05.042]
    14. Bakunova SM, Bakunov SA, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Hall JE, Tidwell RR..  (2007)  Synthesis and in vitro antiprotozoal activity of bisbenzofuran cations.,  50  (23): [PMID:17948982] [10.1021/jm0708634]
    15. Kuettel S, Zambon A, Kaiser M, Brun R, Scapozza L, Perozzo R..  (2007)  Synthesis and evaluation of antiparasitic activities of new 4-[5-(4-phenoxyphenyl)-2H-pyrazol-3-yl]morpholine derivatives.,  50  (23): [PMID:17949068] [10.1021/jm700938n]
    16. Tasdemir D, Topaloglu B, Perozzo R, Brun R, O'Neill R, Carballeira NM, Zhang X, Tonge PJ, Linden A, Rüedi P..  (2007)  Marine natural products from the Turkish sponge Agelas oroides that inhibit the enoyl reductases from Plasmodium falciparum, Mycobacterium tuberculosis and Escherichia coli.,  15  (21): [PMID:17765547] [10.1016/j.bmc.2007.07.032]
    17. Senn M, Gunzenhauser S, Brun R, Séquin U..  (2007)  Antiprotozoal polyacetylenes from the Tanzanian medicinal plant Cussonia zimmermannii.,  70  (10): [PMID:17922552] [10.1021/np0702133]
    18. Bolognesi ML, Lizzi F, Perozzo R, Brun R, Cavalli A..  (2008)  Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activity.,  18  (7): [PMID:18353643] [10.1016/j.bmcl.2008.03.009]
    19. Rodríguez F, Rozas I, Kaiser M, Brun R, Nguyen B, Wilson WD, García RN, Dardonville C..  (2008)  New bis(2-aminoimidazoline) and bisguanidine DNA minor groove binders with potent in vivo antitrypanosomal and antiplasmodial activity.,  51  (4): [PMID:18247550] [10.1021/jm7013088]
    20. Caffrey CR, Steverding D, Swenerton RK, Kelly B, Walshe D, Debnath A, Zhou YM, Doyle PS, Fafarman AT, Zorn JA, Land KM, Beauchene J, Schreiber K, Moll H, Ponte-Sucre A, Schirmeister T, Saravanamuthu A, Fairlamb AH, Cohen FE, McKerrow JH, Weisman JL, May BC..  (2007)  Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.,  51  (6): [PMID:17371810] [10.1128/aac.01418-06]
    21. Bringmann G, Hamm A, Günther C, Michel M, Brun R, Mudogo V..  (2000)  Ancistroealaines A and B, two new bioactive naphthylisoquinolines, and related naphthoic acids from Ancistrocladus ealaensis.,  63  (11): [PMID:11087584] [10.1021/np000247+]
    22. Goclik E, König GM, Wright AD, Kaminsky R..  (2000)  Pelorol from the tropical marine sponge Dactylospongia elegans.,  63  (8): [PMID:10978215] [10.1021/np990502u]
    23. Bringmann G, Dreyer M, Rischer H, Wolf K, Hadi HA, Brun R, Meimberg H, Heubl G..  (2004)  Ancistrobenomine a, the first naphthylisoquinoline oxygenated at Me-3, and related 5,1'-coupled alkaloids, from the "new" plant species ancistrocladusbenomensis.,  67  (12): [PMID:15620251] [10.1021/np0497651]
    24. Bringmann G, Dreyer M, Faber JH, Dalsgaard PW, Staerk D, Jaroszewski JW, Ndangalasi H, Mbago F, Brun R, Reichert M, Maksimenka K, Christensen SB..  (2003)  Ancistrotanzanine A, the first 5,3'-coupled naphthylisoquinoline alkaloid, and two further, 5,8'-linked related compounds from the newly described species Ancistrocladus tanzaniensis.,  66  (9): [PMID:14510589] [10.1021/np030077b]
    25. Schlapper C, Seebacher W, Kaiser M, Brun R, Saf R, Weis R..  (2008)  Epimers of bicyclo[2.2.2]octan-2-ol derivatives with antiprotozoal activity.,  43  (4): [PMID:17698258] [10.1016/j.ejmech.2007.06.007]
    26. Bringmann G, Dreyer M, Faber JH, Dalsgaard PW, Staerk D, Jaroszewski JW, Ndangalasi H, Mbago F, Brun R, Christensen SB..  (2004)  Ancistrotanzanine C and related 5,1'- and 7,3'-coupled naphthylisoquinoline alkaloids from Ancistrocladus tanzaniensis.,  67  (5): [PMID:15165131] [10.1021/np0340549]
    27. Kaiser M, Wittlin S, Nehrbass-Stuedli A, Dong Y, Wang X, Hemphill A, Matile H, Brun R, Vennerstrom JL..  (2007)  Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).,  51  (8): [PMID:17562801] [10.1128/aac.00225-07]
    28. Bakunova SM, Bakunov SA, Patrick DA, Kumar EV, Ohemeng KA, Bridges AS, Wenzler T, Barszcz T, Jones SK, Werbovetz KA, Brun R, Tidwell RR..  (2009)  Structure-activity study of pentamidine analogues as antiprotozoal agents.,  52  (7): [PMID:19267462] [10.1021/jm801547t]
    29. Faist J, Seebacher W, Schlapper C, Kaiser M, Brun R, Saf R, Weis R..  (2009)  Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.,  17  (10): [PMID:19395265] [10.1016/j.bmc.2009.04.002]
    30. Wright AD, Papendorf O, König GM..  (2005)  Ambigol C and 2,4-dichlorobenzoic acid, natural products produced by the terrestrial cyanobacterium Fischerella ambigua.,  68  (3): [PMID:15787461] [10.1021/np049640w]
    31. Busch J, Grether Y, Ochs D, Séquin U..  (1998)  Total synthesis and biological activities of (+)- and (-)-boscialin and their 1'-epimers.,  61  (5): [PMID:9599255] [10.1021/np970517x]
    32. Bringmann G, Messer K, Brun R, Mudogo V..  (2002)  Ancistrocongolines A-D, new naphthylisoquinoline alkaloids from ancistrocladus congolensis.,  65  (8): [PMID:12193010] [10.1021/np010622d]
    33. Schlapper C, Seebacher W, Faist J, Kaiser M, Brun R, Saf R, Weis R..  (2009)  Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates.,  44  (2): [PMID:18571774] [10.1016/j.ejmech.2008.05.002]
    34. Van Miert S, Hostyn S, Maes BU, Cimanga K, Brun R, Kaiser M, Mátyus P, Dommisse R, Lemière G, Vlietinck A, Pieters L..  (2005)  Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.,  68  (5): [PMID:15921407] [10.1021/np0496284]
    35. Bringmann G, Dreyer M, Kopff H, Rischer H, Wohlfarth M, Hadi HA, Brun R, Meimberg H, Heubl G..  (2005)  ent-Dioncophylleine A and related dehydrogenated naphthylisoquinoline alkaloids, the first Asian dioncophyllaceae-type alkaloids, from the "new"plant species Ancistrocladus benomensis.,  68  (5): [PMID:15921410] [10.1021/np049626j]
    36. Kamnaing P, Tsopmo A, Tanifum EA, Tchuendem MH, Tane P, Ayafor JF, Sterner O, Rattendi D, Iwu MM, Schuster B, Bacchi C..  (2003)  Trypanocidal diarylheptanoids from Aframomum letestuianum.,  66  (3): [PMID:12662093] [10.1021/np020362f]
    37. Rodenko B, van der Burg AM, Wanner MJ, Kaiser M, Brun R, Gould M, de Koning HP, Koomen GJ..  (2007)  2,N6-disubstituted adenosine analogs with antitrypanosomal and antimalarial activities.,  51  (11): [PMID:17698622] [10.1128/aac.00425-07]
    38. Berger H, Weis R, Kaiser M, Brun R, Saf R, Seebacher W..  (2008)  Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense.,  16  (12): [PMID:18502136] [10.1016/j.bmc.2008.05.007]
    39. Ge JF, Arai C, Kaiser M, Wittlin S, Brun R, Ihara M..  (2008)  Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives.,  51  (12): [PMID:18476684] [10.1021/jm8003619]
    40. Pontius A, Krick A, Kehraus S, Brun R, König GM..  (2008)  Antiprotozoal activities of heterocyclic-substituted xanthones from the marine-derived fungus Chaetomium sp.,  71  (9): [PMID:18683985] [10.1021/np800294q]
    41. Bakunov SA, Bakunova SM, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Tidwell RR..  (2008)  Synthesis and antiprotozoal activity of cationic 2-phenylbenzofurans.,  51  (21): [PMID:18841956] [10.1021/jm800918v]
    42. Alp M, Göker H, Brun R, Yildiz S..  (2009)  Synthesis and antiparasitic and antifungal evaluation of 2'-arylsubstituted-1H,1'H-[2,5']bisbenzimidazolyl-5-carboxamidines.,  44  (5): [PMID:19010569] [10.1016/j.ejmech.2008.10.003]
    43. Cavalli A, Lizzi F, Bongarzone S, Brun R, Luise Krauth-Siegel R, Bolognesi ML..  (2009)  Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase.,  19  (11): [PMID:19414258] [10.1016/j.bmcl.2009.04.060]
    44. Bakunova SM, Bakunov SA, Wenzler T, Barszcz T, Werbovetz KA, Brun R, Tidwell RR..  (2009)  Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.,  52  (15): [PMID:19606902] [10.1021/jm900805v]
    45. Link A, Heidler P, Kaiser M, Brun R..  (2009)  Synthesis of a series of N6-substituted adenosines with activity against trypanosomatid parasites.,  44  (9): [PMID:19285758] [10.1016/j.ejmech.2009.02.010]
    46. Patrick DA, Bakunov SA, Bakunova SM, Kumar EV, Chen H, Jones SK, Wenzler T, Barzcz T, Werbovetz KA, Brun R, Tidwell RR..  (2009)  Synthesis and antiprotozoal activities of dicationic bis(phenoxymethyl)benzenes, bis(phenoxymethyl)naphthalenes, and bis(benzyloxy)naphthalenes.,  44  (9): [PMID:19409677] [10.1016/j.ejmech.2009.03.014]
    47. Huang Q, Mao J, Wan B, Wang Y, Brun R, Franzblau SG, Kozikowski AP..  (2009)  Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.,  52  (21): [PMID:19817445] [10.1021/jm901112f]
    48. Fotie J, Kaiser M, Delfín DA, Manley J, Reid CS, Paris JM, Wenzler T, Maes L, Mahasenan KV, Li C, Werbovetz KA..  (2010)  Antitrypanosomal activity of 1,2-dihydroquinolin-6-ols and their ester derivatives.,  53  (3): [PMID:20047276] [10.1021/jm900723w]
    49. Bakunov SA, Bakunova SM, Wenzler T, Ghebru M, Werbovetz KA, Brun R, Tidwell RR..  (2010)  Synthesis and antiprotozoal activity of cationic 1,4-diphenyl-1H-1,2,3-triazoles.,  53  (1): [PMID:19928900] [10.1021/jm901178d]
    50. Van Baelen G, Hostyn S, Dhooghe L, Tapolcsányi P, Mátyus P, Lemière G, Dommisse R, Kaiser M, Brun R, Cos P, Maes L, Hajós G, Riedl Z, Nagy I, Maes BU, Pieters L..  (2009)  Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues.,  17  (20): [PMID:19781948] [10.1016/j.bmc.2009.08.057]
    51. Pagliero RJ, Lusvarghi S, Pierini AB, Brun R, Mazzieri MR..  (2010)  Synthesis, stereoelectronic characterization and antiparasitic activity of new 1-benzenesulfonyl-2-methyl-1,2,3,4-tetrahydroquinolines.,  18  (1): [PMID:19942439] [10.1016/j.bmc.2009.11.010]
    52. Holloway GA, Parisot JP, Novello PM, Watson KG, Armstrong T, Thompson RC, Street IP, Baell JB..  (2010)  Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi.,  20  (6): [PMID:20185305] [10.1016/j.bmcl.2010.02.022]
    53. Breuning A, Degel B, Schulz F, Büchold C, Stempka M, Machon U, Heppner S, Gelhaus C, Leippe M, Leyh M, Kisker C, Rath J, Stich A, Gut J, Rosenthal PJ, Schmuck C, Schirmeister T..  (2010)  Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids.,  53  (5): [PMID:20131843] [10.1021/jm900946n]
    54. Watts KR, Ratnam J, Ang KH, Tenney K, Compton JE, McKerrow J, Crews P..  (2010)  Assessing the trypanocidal potential of natural and semi-synthetic diketopiperazines from two deep water marine-derived fungi.,  18  (7): [PMID:20303767] [10.1016/j.bmc.2010.02.034]
    55. Machon U, Büchold C, Stempka M, Schirmeister T, Gelhaus C, Leippe M, Gut J, Rosenthal PJ, Kisker C, Leyh M, Schmuck C..  (2009)  On-bead screening of a combinatorial fumaric acid derived peptide library yields antiplasmodial cysteine protease inhibitors with unusual peptide sequences.,  52  (18): [PMID:19715342] [10.1021/jm900629w]
    56. Ngantchou I, Nyasse B, Denier C, Blonski C, Hannaert V, Schneider B..  (2010)  Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei.,  20  (12): [PMID:20529682] [10.1016/j.bmcl.2010.04.145]
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    89. Liew LP, Kaiser M, Copp BR..  (2013)  Discovery and preliminary structure-activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds.,  23  (2): [PMID:23265884] [10.1016/j.bmcl.2012.11.072]
    90. McKeever C, Kaiser M, Rozas I..  (2013)  Aminoalkyl derivatives of guanidine diaromatic minor groove binders with antiprotozoal activity.,  56  (3): [PMID:23301592] [10.1021/jm301614w]
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    152. Unpublished dataset, 
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